Wang Delong, Ren Shuangxi, Wang Hao, Yan He, Feng Juntao, Zhang Xing
Research & Development Center of Biorational Pesticide, Key Laboratory of Plant Protection Resources and Pest Management of Ministry of Education, Northwest A&F University, Yangling 712100, P. R. China (phone: +86-29-87092122; fax: +86-29-87093344 or phone: +86-29-87091884; fax: +86-29-87092122).
Chem Biodivers. 2014 Jun;11(6):886-903. doi: 10.1002/cbdv.201300212.
To continuously improve the potential utility of the natural lead compound of carabrone in agrochemistry, carabrone oxime and 36 novel oxime ester derivatives of carabrone modified at C(4) were synthesized, and evaluated for their antifungal activities against Botrytis cinerea in vitro and in vivo. Of these 36 oxime ester derivatives, some compounds exhibited antifungal activities in vitro or in vivo. It was found that compounds with a pyridinyl residue can either efficiently inhibit spore germination or efficiently inhibit hyphal growth of B. cinerea, and compound 9 exhibited the highest activity in vitro and in vivo with IC50 and EC50 values of 1.17 and 12.9 μg/ml, respectively. Further, the structure-activity relationships are also discussed.
为持续提高卡拉布酮天然先导化合物在农业化学中的潜在效用，合成了卡拉布酮肟及36种在C(4)位修饰的卡拉布酮新型肟酯衍生物，并对其体外和体内抗灰葡萄孢菌的活性进行了评估。在这36种肟酯衍生物中，一些化合物在体外或体内表现出抗真菌活性。研究发现，带有吡啶基残基的化合物既能有效抑制灰葡萄孢菌的孢子萌发，也能有效抑制其菌丝生长，化合物9在体外和体内均表现出最高活性，其IC50和EC50值分别为1.17和12.9μg/ml。此外，还讨论了构效关系。
